SOLID DISPERSION OF NEBIVOLOL HYDROCHLORIDE IMPREGNATED BUCCAL PATCH: FORMULATION AND CHARACTERIZATION
Keywords:Nebivolol hydrochloride (NBH), Mucoadhesive buccal patch, HPMC K 15 M
Objective: The objective of the present investigation was to design and characterize a mucoadhesive buccal patch of Nebivolol hydrochloride in order to administer a small dose of a drug to treat hypertension effectively and thereby avoiding disadvantages such as patient noncompliance and low bioavailability.
Methods: The buccal patches were prepared by solvent casting method. The polymers used to formulate patches were HPMC K 15 M, PVP K 30, and propylene glycol was used as plasticizer and ethanol as the solvent. The drug-polymer compatibility studied was conducted by FTIR.
Results: All the developed Patches had good transparency and stability. All formulated patches showed pH in the range of 6.49 to 7.22, and drug content was more than 90%. The folding endurance value showed that the patches are flexible and non-brittle. The in vitro residence time was found to more than 30 min. Thickness, % moisture absorption, and % moisture loss values were in a normal range. The drug release study was conducted for 8 h, and it was found drug release was decreased with the increase in polymer concentration. The in vitro release profiles of the drug from all the formulations appeared to follow Korsmeyer Peppa's exponential model, and release exponent (n) was found to be more than 0.45 so that the release can be characterized by Non–Fickian (anomalous) diffusion.
Conclusion: From the results, it was concluded that drug released from formulated buccal patches follows sustained release pattern, Hence can be used for the treatment of the hypertensive patient.
Weber MA, Schiffrin EL, White WB, Mann S, Lindholm LH, Kenerson JG, et al. Clinical practice guidelines for the management of hypertension in the community: a statement by the American society of hypertension and the international society of hypertension. J Hypertens 2014;32:3-15.
Kearney PM, Whelton M, Reynolds K, Whelton PK, He J. Worldwide prevalence of hypertension: a systematic review. J hypertens 2004;22:11-9.
Gavhane YN, Yadav AV. Loss of orally administered drugs in GI tract. Saudi Pharm J 2012;20:331-44.
Harris D, Robinson JR. Drug delivery via the mucous membrane of the oral cavity. J Pharm Sci 1992;81:1-10.
Tarun P, Kumar V, Kumar A. Drug delivery via the buccal patch-a novel approach. Indo Am J Pharm Res 2013;3:3466-83.
Veverka A, Nuzum DS, Jolly JL. Nebivolol: a third-generation β-adrenergic blocker. Ann Pharmacother 2006;40:1353-60.
Shah I, Bhatt S, Yadav A. Enhancement of solubility and dissolution of nebivolol by solid dispersion technique. Int J Pharm Pharm Sci 2014;6:566-71.
Shah H, Shah V, Bhutani S, Parikh D, Mehta T. Dissolution improvement of nebivolol hydrochloride using solid dispersion adsorbate technique. Asian J Pharm 2015;9:49-55.
Hirlekar RS. Design of buccal drug delivery system for a poorly soluble drug. Asian J Pharm Clin Res 2009;2:49-53.
Periolia L, Ambrogia V, Angelicia F, Riccia M, Giovagnolia S, Capuccellab M, Rossi C. Development of mucoadhesive patches for buccal administration of ibuprofen. J Controlled Release 2004;9:73-82.
Priya S, Rathnanand M, Udupa N, Ongole R, Sumanth KN, Joshi U. Preparation and evaluation of buccal mucoadhesive patch of betamethasone sodium phosphate for the treatment of oral submucous fibrosis. J Chem Pharm Res 2011;3:56-65.
Patel VM, Prajapati BG, Patel MM. Design and in vitro characterization of eudragit containing mucoadhesive buccal patches. Int J Pharm Tech Res 2009;1:783-9.
Averineni RK, Sunderajan SG, Mutalik S, Nayak U, Shavi G, Armugam K, et al. Development of mucoadhesive buccal films for the treatment of oral sub-mucous fibrosis: a preliminary study. Pharm Dev Technol 2009;14:199–207.
Deshpande PB, Dandagi P, Udupa N, Shavi VG, Jain SS, Vasanth SG. Controlled release polymeric ocular delivery of acyclovir. Pharm Dev Technol 2009;15:369-78.
Thakur P, Ratnaparkhi MP. Formulation and evaluation of mouth dissolving film of felodipine. Res J Pharm Technol 2014;7:1145-9.
Wani MS, Dehghan MH, Mahendrakumar C, Polshettiwar SA, Yadav VB. Design and evaluation of terbutaline sulphate buccal patch. Res J Pharm Technol 2009;2:86-90.
Singhvi G, Singh M. Review: in vitro drug release charecterization models. Int J Pharm Sci Res 2011;2:77-84.
Moffat AC, Osselton MD, Brain W. Clarke's analysis of drugs and poisons overview. 3rd Edition. Pharmaceutical Press: Londom; 2009.
Gupta JRD, Irchhiaya R, Garud N, Tripathi P, Dubey P, Patel JR. Formulation and evaluation of matrix type transdermal patches of glibenclamide. Int J Pharm Sci Drug Res 2009;1:46-50.
Gawai N, Zaheer Z. Formulation and development of mucoadhesive sustained release buccal tablets and patches of 5-fluorouracil using different polymers. Asian J Pharm Clin Res 2018;11:174-85.
Patel RS, Poddar SS. Development and characterization of mucoadhesive buccal patches of salbutamol sulphate. Curr Drug Delivery 2009;6:140-4.
Ashutosh R, Prabhakara P, Akhilesh D. Design and evaluation of buccal patches containing combination of hydrochlorothiazide and atenolol. Int J Appl Pharm 2018;10:105-12.
Soji S, Arun JL. Development, evaluation, and characterization of Losartan potassium buccal patches using jackfruit polymer. Asian J Pharm Clin Res 2019;12:24-30.